酸枣仁总皂苷抗抑郁作用的实验研究

目的研究酸枣仁总皂苷对行为绝望小鼠抑郁模型的影响。方法采用小鼠强迫游泳实验和悬尾实验抑郁模型,小鼠行为绝望的不动时间作为指标,考察酸枣仁总皂苷抗抑郁活性。结果酸枣仁总皂苷中、高剂量组均能减少小鼠强迫游泳和悬尾不动时间,与空白对照组比较差异有统计学意义(P<0.05,P<0.01)。结论酸枣仁总皂苷具有一定的抗抑郁作用。     

百合皂苷的提取工艺与抗抑郁作用研究

目的:研究百合皂苷的提取工艺与抗抑郁作用。方法:以乙醇体积分数、乙醇用量、提取时间为考察因素,以百合皂苷提取率为指标,通过L9(34)正交试验优选百合皂苷提取工艺。将小鼠分为正常对照(等容生理盐水)组、氟西汀(0.004 g/kg)组与百合皂苷高、中、低剂量(0.100、0.050、0.025 g/kg)组。悬尾实验和强迫游泳实验均记录小鼠4 min内不动时间;拮抗利血平降低小鼠体温实验中记录复制模型4 h后小鼠体温。结果:百合皂苷最佳提取工艺为加入1倍量的70%乙醇,提取3 h。与正常对照组比较,百合皂苷提取物高、中剂量组小鼠4 min内悬尾不动时间、游泳不动时间均缩短,差异均有统计学意义(P<0.05);复制模型4 h后小鼠体温变化减小,差异有统计学意义(P<0.05)。结论:百合皂苷具有一定的抗抑郁作用。     

正交试验优选茅莓总皂苷的提取工艺

目的:优选茅莓总皂苷的提取工艺。方法:在单因素考察的基础上,以乙醇浓度、固液比、提取温度和提取时间为考察因素,以茅莓总皂苷提取率为指标,优选茅莓总皂苷的提取工艺。结果:最佳提取工艺为乙醇浓度80%,提取时间为3h,固液比为1:20,提取温度为80℃。在此条件下,茅莓总皂苷提取率达到1.994%。结论:该工艺稳定、可行,可为工业化生产提供理论依据。     

建立萝藦总皂苷的提取纯化及含量测定的方法

目的探讨提取萝藦中总皂苷的方法并确定纯化树脂类型并做含量测定,研究其药用价值。方法使用乙醇提取萝藦中总皂苷,研究各变量对提取效果的影响,采用正交实验;比较所供四种树脂的吸附力,指标为总皂苷含量,选取最优;以薯蓣皂苷为标准,采用分光光度法,计算萝藦总皂苷的含量。结果最优提取方案为,乙醇浓度80%,料液比1:8,温度70℃,时间1.5h;D101大孔吸附树脂效果最好;萝藦总皂苷含量为15.9%。结论乙醇浓度,提取温度对萝藦皂苷的提取影响较大,优选出的最佳提取工艺条件及纯化总皂苷的方法对萝藦皂苷进一步开发有很好的参考价值。     

湖北恩施产三七总皂苷的提取工艺研究

目的优化超声法提取三七总皂苷工艺。方法采用Box-Benhnken设计优化三七总皂苷超声提取工艺。结果优化的提取工艺参数为:乙醇体积分数72%、固液比1∶11、提取时间12min。在此工艺条件下三七总皂苷的提取率为6.92%,与模型预测值6.97%基本相符。结论超声提取法是一种高效提取恩施三七总皂苷的有效方法。     

芦笋食用与废弃部分皂苷含量的比较研究

目的优化芦笋皂苷提取工艺,比较芦笋食用部分和废弃部分的皂苷含量。方法采用超声提取法,以芦笋中皂苷的提取率为指标,采用单因素实验和正交实验考察乙醇浓度、料液比、提取时间和提取温度对超声法提取芦笋两部分中总皂苷的影响,并用紫外分光光度法测定皂苷在两部分中的含量。结果芦笋食用部分总皂苷最佳提取条件为提取温度为70℃,提取时间为2h,料液比为1：15,乙醇浓度为10％。提取率为179．83mg·g-1;芦笋废弃部分总皂苷最佳提取条件为提取温度为40℃,提取时间为2．5h,料液比为1：15,乙醇浓度为30％,提取率为117．8lmg·g-1。结论经SPSS软件进行独立样本T检验,得知芦笋食用与废弃部分粗提物中皂苷的含量差异较大,需待进一步进行研究。     

岗梅叶总皂苷的提取纯化工艺研究

目的优选岗梅叶总皂苷的提取、纯化工艺,为生产提供依据。方法以人参皂苷Re作为含量测定对照品,岗梅叶总皂苷洗脱率为评价指标,采用L9(34)正交试验设计优选岗梅叶总皂苷的最佳提取工艺。结果最佳提取工艺为20倍量60%的乙醇,70℃下超声提取60 min,采用D-101型大孔树脂,以100 ml蒸馏水洗去水溶性杂质,50%的乙醇75 ml洗脱总皂苷的效果好。结论验证实验表明优选出的提取工艺稳定可行,适用于岗梅叶总皂苷的提取、纯化。     

均匀设计优化三七总皂苷提取工艺

目的优选三七总皂苷提取工艺的最佳条件。方法通过均匀设计试验。结果提取溶剂用量为药材重量的 1 3倍 ,乙醇浓度为 30 % ,提取温度为 70℃ ,加热时间 4 0min,同法提取 2次 ,三七总皂苷平均提取率为 94 92 %。结论三七总皂苷提取率高、生产成本低 ,适合工业生产。     

人参总皂苷对小鼠的抗抑郁作用

目的：初步探讨人参总皂苷对小鼠的抗抑郁作用。方法：选取健康雄性昆明种小鼠,随机分为5组,空白对照组、阳性药组、人参总皂苷125、250、500 mg.kg^-1剂量组。通过小鼠自主活动实验、小鼠强迫游泳实验和小鼠悬尾实验,观察人参总皂苷对小鼠抗抑郁作用的影响。结果：各给药组小鼠自主活动行为与空白对照组比较均无明显差异;人参总皂苷125、250、500 mg.kg-1均可以显著缩短小鼠强迫游泳及小鼠悬尾不动时间。结论：实验结果表明人参总皂苷在小鼠＂行为绝望＂模型中有一定的抗抑郁作用。     

新疆核桃分心木总皂苷的提取纯化工艺研究

目的优选核桃分心木总皂苷的最佳提取纯化工艺。方法以齐墩果酸为对照品,利用紫外可见分光光度法测定核桃分心木中的总皂苷含量;利用单因素实验结果设计正交实验,考察了乙醇体积分数、提取时间、料液比和提取次数对核桃分心木总皂苷提取率的影响;利用大孔吸附树脂对核桃分心木总皂苷进行纯化工艺研究。结果最佳提取工艺为:加25倍量体积分数80%乙醇,80℃回流提取2次,每次2h;最佳纯化工艺为:采用D101大孔吸附树脂,最大上样量为180mL,水洗脱量8BV,洗脱剂体积分数50%乙醇,洗脱体积7BV。结论该法简易可行,效果较佳。     

Synthesis,Cytotoxicity and Antileishmanial Activity of Some N-(2-(indol-3-yl)ethyl)-7-chloroquinolin-4-amines

We report herein the condensation of 4,7-dichloroquinoline (1) with tryptamine (2) and D-tryptophan methyl ester (3) . Hydrolysis of the methyl ester adduct (5) yielded the free acid (6) . The compounds were evaluated in vitro for activity against four different species of Leishmania promastigote forms and for cytotoxic activity against Kb and Vero cells. Compound (5) showed good activity against the Leishmania species tested, while all three compounds displayed moderate activity in both Kb and Vero cells.     

Efficacy of gut lavage,hemodialysis, and hemoperfusion in the therapy of paraquat or diquat intoxication

Clinical and in vitro investigations were carried out to test the efficacy of gut lavage, hemodialysis, and hemoperfusion in the treatment of poisoning with paraquat or diquat. In a patient suffering from diquat intoxication 130 times more diquat was removed by gut lavage 30 h after ingestion than was removed by complete aspiration of the gastric contents.Determination of in vitro clearances for paraquat and diquat by hemodialysis showed that, at serum concentrations of 1–2 ppm, such as are frequently encountered in poisoning in man, toxicologically relevant quantities of herbicide cannot be removed from the body. At a concentration of 20 ppm, on the other hand, hemodialysis proved to be effective, the clearance being 70 ml/min at a blood flow rate of 100 ml/min. The efficacy of hemoperfusion with coated activated charcoal was on the whole better. Especially at concentrations around 1–2 ppm, the clearance values for hemoperfusion were some 5–7 times higher than those for hemodialysis.In a patient suffering from paraquat poisoning, both hemodialysis as well as hemoperfusion were carried out. The in vitro results could be confirmed: At serum concentrations of paraquat less than 1 ppm no clearance could be obtained by hemodialysis while by hemoperfusion with activated charcoal quite high clearance values were measured and the serum level dropped down to zero.

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Zusammenfassung Klinische Untersuchungen und Laboratoriumsversuche wurden durchgeführt, um die Wirksamkeit von Darmspülung, Hämodialyse und Hämoperfusion bei Paraquat- und Deiquat-Vergiftungen zu prüfen.Bei einem Patienten wurde 30 Std nach Deiquat-Aufnahme durch Darmspülung 130mal mehr Deiquat entfernt als durch vollständige Aspiration des Mageninhaltes. In vitro-Versuche ergaben, daß bei Blutserumkonzentrationen von 1–2 ppm, die bei Vergiftungen oft gemessen werden, durch Hämodialyse keine toxikologisch relevanten Paraquat- oder Deiquat-Mengen entfernt werden können. Dagegen erwies sich die Hämodialyse bei 20 ppm und einer Blutumlaufgeschwindigkeit von 100 ml/min mit einer Clearance von 70 ml/min als wirksam. Die Hämoperfusion mit beschicheter Aktivkohle war in diesen Versuchen aber eindeutig überlegen, denn insbesondere bei Konzentrationen um 1–2 ppm waren die Clearance-Werte 5–7mal höher als bei der Hämodialyse.Die in vitro-Ergebnisse wurden bei einem Patienten mit einer Paraquat-Vergiftung bestätigt: Bei Konzentrationen unter 1 ppm war die Hämodialyse wirkungslos, während durch Hämoperfusion relativ hohe Clearance-Werte erreicht wurden, so daß der Serumspiegel rasch unter die Nachweisgrenze abfiel.

     

In vitro studies on sterically stabilized liposomes (SL) as enzyme carriers in organophosphorus (OP) antagonism

This study describes a new approach for organophosphorous (OP) antidotal treatment by encapsulating an OP hydrolyzing enzyme, OPA anhydrolase (OPAA), within sterically stabilized liposomes. The recombinant OPAA enzyme was derived from Alteromonas strain JD6. It has broad substrate specificity to a wide range of OP compounds: DFP and the nerve agents, soman and sarin. Liposomes encapsulating OPAA (SL)* were made by mechanical dispersion method. Hydrolysis of DFP by (SL)* was measured by following an increase of fluoride ion concentration using a fluoride ion selective electrode. OPAA entrapped in the carrier liposomes rapidly hydrolyze DFP, with the rate of DFP hydrolysis directly proportional to the amount of (SL)* added to the solution. Liposomal carriers containing no enzyme did not hydrolyze DFP. The reaction was linear and the rate of hydrolysis was first order in the substrate. This enzyme carrier system serves as a biodegradable protective environment for the recombinant OP-metabolizing enzyme, OPAA, resulting in prolongation of enzymatic concentration in the body. These studies suggest that the protection of OP intoxication can be strikingly enhanced by adding OPAA encapsulated within (SL)* to pralidoxime and atropine.     

Lung disease and PKCs

The lung offers a rich opportunity for development of therapeutic strategies focused on isozymes of protein kinase C (PKCs). PKCs are important in many cellular responses in the lung, and existing therapies for pulmonary disorders are inadequate. The lung poses unique challenges as it interfaces with air and blood, contains a pulmonary and systemic circulation, and consists of many cell types. Key structures are bronchial and pulmonary vessels, branching airways, and distal air sacs defined by alveolar walls containing capillaries and interstitial space. The cellular composition of each vessel, airway, and alveolar wall is heterogeneous. Injurious environmental stimuli signal through PKCs and cause a variety of disorders. Edema formation and pulmonary hypertension (PHTN) result from derangements in endothelial, smooth muscle (SM), and/or adventitial fibroblast cell phenotype. Asthma, chronic obstructive pulmonary disease (COPD), and lung cancer are characterized by distinctive pathological changes in airway epithelial, SM, and mucous-generating cells. Acute and chronic pneumonitis and fibrosis occur in the alveolar space and interstitium with type 2 pneumocytes and interstitial fibroblasts/myofibroblasts playing a prominent role. At each site, inflammatory, immune, and vascular progenitor cells contribute to the injury and repair process. Many strategies have been used to investigate PKCs in lung injury. Isolated organ preparations and whole animal studies are powerful approaches especially when genetically engineered mice are used. More analysis of PKC isozymes in normal and diseased human lung tissue and cells is needed to complement this work. Since opposing or counter-regulatory effects of selected PKCs in the same cell or tissue have been found, it may be desirable to target more than one PKC isozyme and potentially in different directions. Because multiple signaling pathways contribute to the key cellular responses important in lung biology, therapeutic strategies targeting PKCs may be more effective if combined with inhibitors of other pathways for additive or synergistic effect. Mechanisms that regulate PKC activity, including phosphorylation and interaction with isozyme-specific binding proteins, are also potential therapeutic targets. Key isotypes of PKC involved in lung pathophysiology are summarized and current and evolving therapeutic approaches to target them are identified.     

Steroidal sapogenin contents in some domestic plants

In order to find out the values of the steroid resources for the future use. the compositions and contents of steroidal sapogenins from 13 domestic plants have been investigated. As a result,Dioscorea nipponica, D. quinqueloba andSmilax china were found to have large amount of diosgenin. And pennogenin inTrillium kamtschaticum andParis verticillata, yuccagenin inAllium fistulosum, hecogenin inAgave americana and neochlorogenin inSolanum nigum were appeared to be major steroidal sapogenins.